Dalcetrapib
Dalcetrapib does not affect the pharmacokinetics of a combined oral contraceptive in a crossover trial (Int J Clin Pharmacol Ther 2012)
Original title: No clinically relevant drug-drug interactions when dalcetrapib is co-administered with a monophasic oral contraceptive (Microgynon® 30)
A randomized, open-label, two-period crossover study in healthy women assessed whether dalcetrapib affects the pharmacokinetics and ovulation-suppressing ability of the monophasic oral contraceptive Microgynon 30. After a run-in period, 30 subjects took Microgynon 30 daily for 21 days with or without dalcetrapib 900 mg daily for days 1 to 14. The geometric mean ratios for ethinylestradiol exposure were 92% and 105% for area under the curve and maximum concentration, and for levonorgestrel 92% and 93%, all with 90% confidence intervals close to the no-effect range. Luteinizing hormone, follicle stimulating hormone, estrogen, and progesterone concentrations were comparable between treatments, indicating dalcetrapib has no clinically relevant effect on contraceptive pharmacokinetics or efficacy.
Original abstract
Unlabelled: Dalcetrapib, a cholesteryl ester transfer protein modulator, under development to increase high-density lipoprotein cholesterol and potentially decrease cardiovascular risk, will potentially be co-prescribed to women on oral contraceptive (OC).
Objective: Assess the effect of dalcetrapib on the pharmacokinetics and ability to suppress ovulation of Microgynon® 30, a representative monophasic OC.
Materials And Methods: A single-center, randomized, open-label, two-period crossover study in healthy women receiving monophasic OC. Subjects received Microgynon® 30 (ethinylestradiol 0.03 mg/levonorgestrel 0.15 mg) once daily for 21 days followed by 7 treatment-free days (run-in period), then were randomized to Microgynon® 30 daily for 21 days with or without dalcetrapib 900 mg daily for Day 1 - 14. Plasma ethinylestradiol and levonorgestrel were measured on Day 14, and luteinizing hormone, follicle stimulating hormone, progesterone and estrogen from Day 11 - 14. The primary endpoint plasma exposure (AUC0-24 and Cmax) on Day 14 was evaluated for ethinylestradiol and levonorgestrel. Safety was monitored throughout.
Results: 30 subjects were randomized. The exposure of ethinylestradiol and levonorgestrel was similar when Microgynon® 30 was administered with or without dalcetrapib; for ethinylestradiol the geometric mean ratio %, (90% confidence interval (CI)) for AUC0-24 and Cmax were 92 (86 - 98) and 105 (95 - 115) and for levonorgestrel 92 (88 - 96) and 93 (87 - 99), respectively. Concentrations of luteinizing hormone, follicle stimulating hormone, estrogen and progesterone were comparable between treatments.
Conclusions: Dalcetrapib has no clinically relevant effect on the pharmacokinetics of ethinylestradiol and levonorgestrel. Contraceptive efficacy of Microgynon® 30 is not anticipated to be compromised by co-administration of dalcetrapib.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.